ADAMTS-5 Inhibitor
Based on 4 publication(s) in Google Scholar
ADAMTS-5 Inhibitor is a potent ADAMTS-5 (aggrecanase-2) inhibitor, with an IC50 of 1.1 µM. ADAMTS-5 Inhibitor shows >40-fold functional selectivity over ADAMTS-4 (aggrecanase-1).
For research use only. We do not sell to patients.
- Purity: 99.59%
- CAS No.: 929634-33-3
- Formula: C16H11ClF3N3OS3
- Molecular Weight:449.92
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Covalent Screening Library
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Publications Citing Use of MedChemExpress (MCE) ADAMTS-5 Inhibitor
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Biological Activity
ADAMTS-5 (aggrecanase-2) is an extracellular matrix-degrading protease implicated in cartilage destruction in arthritis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 929634-33-3
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Appearance Solid
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Molecular Weight 449.92
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Formula C16H11ClF3N3OS3
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Color Light yellow to yellow
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SMILES
O=C1NC(S/C1=C\C2=C(SCC3=CC=C(Cl)C=C3)N(C)N=C2C(F)(F)F)=S
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Atherosclerosis
2025 May:404:119190. PMID: 40215897 -
Exp Eye Res
ADAMTS5 promotes neovascularization via autophagic degradation of PEDF in proliferative diabetic retinopathy. [Abstract]2023 Sep:234:109597. PMID: 37490993 -
Theriogenology
Eif2s3y alleviated LPS-induced damage to mouse testis and maintained spermatogenesis by negatively regulating Adamts5. [Abstract]2023 Nov:211:65-75. PMID: 37586163 -
Solvent & Solubility
DMSO : 83.33 mg/mL (185.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.62 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.62 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Gilbert AM, et al. 5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1189-92. [Content Brief]
[2]. Wylie JD, et al. Adamts5 (aggrecanase-2) is widely expressed in the mouse musculoskeletal system and is induced in specific regions of knee joint explants by inflammatory cytokines. J Orthop Res. 2012 Feb;30(2):226-33. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2226 mL | 11.1131 mL | 22.2262 mL | 55.5654 mL |
| 5 mM | 0.4445 mL | 2.2226 mL | 4.4452 mL | 11.1131 mL | |
| 10 mM | 0.2223 mL | 1.1113 mL | 2.2226 mL | 5.5565 mL | |
| 15 mM | 0.1482 mL | 0.7409 mL | 1.4817 mL | 3.7044 mL | |
| 20 mM | 0.1111 mL | 0.5557 mL | 1.1113 mL | 2.7783 mL | |
| 25 mM | 0.0889 mL | 0.4445 mL | 0.8890 mL | 2.2226 mL | |
| 30 mM | 0.0741 mL | 0.3704 mL | 0.7409 mL | 1.8522 mL | |
| 40 mM | 0.0556 mL | 0.2778 mL | 0.5557 mL | 1.3891 mL | |
| 50 mM | 0.0445 mL | 0.2223 mL | 0.4445 mL | 1.1113 mL | |
| 60 mM | 0.0370 mL | 0.1852 mL | 0.3704 mL | 0.9261 mL | |
| 80 mM | 0.0278 mL | 0.1389 mL | 0.2778 mL | 0.6946 mL | |
| 100 mM | 0.0222 mL | 0.1111 mL | 0.2223 mL | 0.5557 mL |
ADAMTS-5 Inhibitor Related Classifications
HY-114996 Related Classifications
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